Preparation and characterization of naringenin microparticles via a supercritical anti-Solvent process

Naringenin (NAR) exhibits many biological and pharmacological activities. However, its poor water-solubility and dissolution rate restrict its oral-intestinal absorption rate and bioavailability. In order to improve its dissolution rate, micronized NAR was successfully prepared using a supercritical anti-solvent process. A mixed acetone/dichloromethane solution and CO 2 were used as the solvent and anti-solvent, respectively. The optimal temperature (35   °C), pressure (12   MPa), drug concentration (15   mg/mL), solution flow rate (1   mL/min), and volume percentage of dichloromethane (45%) were determined using a single-factor method. Under optimal conditions, a mean particle size of 611   ±   32   nm was obtained. XRD and FTIR analyses indicated that the unprocessed NAR and micronized NAR using solution-enhanced dispersion by supercritical CO 2 (SEDS) processes exhibited the same crystal structure and chemical structure, and the samples showed similar DSC thermograms. An in vitro dissolution test showed that micronization significantly enhanced the dissolution of NAR.